摘要
黄酮类是众所周知的抗多种病原微生物的抗菌药物。随着抗生素耐药性细菌引起的无法治愈的感染的流行,黄酮类化合物由于其成为抗生素替代品的潜能而吸引了诸多兴趣。本文总结了黄酮类化合物作为抗菌药物的构效关系,讨论了黄酮类抗菌机制的最新进展。结果表明:黄酮类芳香环上的特定位点的羟基可提高活性。然而,活性羟基基团的甲基化通常减低活性。A环的亲油性对查尔酮的活性至关重要。疏水取代基如异戊二烯基、氨烷基链、烷基链、氮杂环或氧杂环通常增强所有黄酮类的活性。推测的黄酮类抗菌机制如下:抑制核酸合成、抑制胞质膜功能、抑制能量代谢、抑制附着物和生物膜的形成、抑制细胞膜上的孔蛋白、改变膜通透性和致病性的衰减。
关键词: 抗菌活性,黄酮类,机制,构效关系。
Current Medicinal Chemistry
Title:Antibacterial Activities of Flavonoids: Structure-Activity Relationship and Mechanism
Volume: 22 Issue: 1
Author(s): Yixi Xie, Weijie Yang, Fen Tang, Xiaoqing Chen and Licheng Ren
Affiliation:
关键词: 抗菌活性,黄酮类,机制,构效关系。
摘要: Flavonoids are well known as antibacterial agents against a wide range of pathogenic microorganism. With increasing prevalence of untreatable infections induced by antibiotic resistance bacteria, flavonoids have attracted much interest because of the potential to be substitutes for antibiotics. In this review, the structure-relationship of flavonoids as antibacterial agents is summarized, and the recent advancements on the antibacterial mechanisms of flavonoids are also discussed. It is concluded that hydroxyls at special sites on the aromatic rings of flavonoids improve the activity. However, the methylation of the active hydroxyl groups generally decreases the activity. Besides, the lipopholicity of the ring A is vital for the activity of chalcones. The hydrophobic substituents such as prenyl groups, alkylamino chains, alkyl chains, and nitrogen or oxygen containing heterocyclic moieties usually enhance the activity for all the flavonoids. The proposed antibacterial mechanisms of flavonoids are as follows: inhibition of nucleic acid synthesis, inhibition of cytoplasmic membrane function, inhibition of energy metabolism, inhibition of the attachment and biofilm formation, inhibition of the porin on the cell membrane, alteration of the membrane permeability, and attenuation of the pathogenicity.
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Cite this article as:
Yixi Xie, Weijie Yang, Fen Tang, Xiaoqing Chen and Ren Licheng, Antibacterial Activities of Flavonoids: Structure-Activity Relationship and Mechanism, Current Medicinal Chemistry 2015; 22 (1) . https://dx.doi.org/10.2174/0929867321666140916113443
DOI https://dx.doi.org/10.2174/0929867321666140916113443 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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